famitinib: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 16662431 |
| CHEMBL ID | 1278146 |
| SCHEMBL ID | 137251 |
| MeSH ID | M0588957 |
| Synonym |
|---|
| (z)-2-(5-fluoro-2-oxo-1,2-dihydroindol-3-ylidenemethyl)-5-(2-diethylaminoethyl)-3-methyl-1,5,6,7-tetrahydropyrrolo-[3,2-c]pyridin-4-one |
| shr-1020 |
| bdbm50331023 |
| shr1020 |
| CHEMBL1278146 , |
| famitinib |
| unii-768fw21j3l |
| 1044040-56-3 |
| famitinib, (z) |
| 5-(2-(diethylamino)ethyl0-2-9(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl)-3-methyl-6,7-dihydro-1h-pyrrolo(3,2-c)pyridin-4(5h)-one |
| 768fw21j3l , |
| 4h-pyrrolo(3,2-c)pyridin-4-one, 5-(2-(diethylamino)ethyl)-2-((z)-(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-1,5,6,7-tetrahydro-3-methyl- |
| famitinib [inn] |
| (z)-5-(2-(diethylamino)ethyl)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-3-methyl-6,7-dihydro-1h-pyrrolo(3,2-c)pyridin-4(5h)-one |
| 4h-pyrrolo(3,2-c)pyridin-4-one, 5-(2-(diethylamino)ethyl)-2-((5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-1,5,6,7-tetrahydro-3-methyl- |
| famitinib [who-dd] |
| 945380-27-8 |
| shr 1020 |
| compound 9 [pmid: 21028894] |
| 5-(2-diethylaminoethyl)-2-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1h-pyrrolo[4,5-c]pyridin-4-one |
| gtpl7886 |
| SCHEMBL137251 |
| DB11741 |
| Q27077275 |
| (z)-5-(2-(diethylamino)ethyl)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-3-methyl-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one |
| 5-(2-(diethylamino)ethyl)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-3-methyl-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one |
| 5-[2-(diethylamino)ethyl]-2-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1h-pyrrolo[3,2-c]pyridin-4-one |
| MS-27081 |
| EX-A6762 |
| STARBLD0044024 |
Famitinib is a tyrosine kinase inhibitor targeting VEGFR2, PDGFR, and c-kit. It is under clinical investigation for the treatment of solid tumors.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Famitinib-related TSH increase may be an early indicator of its efficacy." | ( Hypothyroidism as a potential biomarker of efficacy of famitinib, a novel VEGFR-2 inhibitor in metastatic breast cancer. Cao, J; Hu, X; Lv, F; Wang, B; Wang, L; Wang, Z; Zhang, J, 2014) | 1.37 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The most common ≥grade 3 treatment-related adverse events were hypertension (32." | ( Antitumor activity and safety of camrelizumab plus famitinib in patients with platinum-resistant recurrent ovarian cancer: results from an open-label, multicenter phase 2 basket study. Gao, Y; Hu, W; Lou, G; Pan, M; Peng, J; Shi, H; Sun, R; Wang, L; Wang, Q; Wu, X; Xia, L; Zhang, Y; Zhou, Q; Zhou, X; Zhu, J, 2022) | 0.97 |
This study is to establish physiologically based pharmacokinetic (PBPK) models of famitinib in rat and monkey. The aim is to predict the pharmacokinetics and tissue distribution of fam it in human based on the PBPK models.
HS-10296 and famitinib exhibit significant synergistic antitumor activity. Third-generation EGFR inhibitor combined with VEGFR inhibitor provides a promising strategy in the treatment of EGFR-mutant NSCLC.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Collectively, our results indicate that HS-10296 and famitinib exhibit significant synergistic antitumor activity, suggesting that the third-generation EGFR inhibitor combined with VEGFR inhibitor provides a promising strategy in the treatment of EGFR-mutant NSCLC." | ( Third-generation EGFR inhibitor HS-10296 in combination with famitinib, a multi-targeted tyrosine kinase inhibitor, exerts synergistic antitumor effects through enhanced inhibition of downstream signaling in EGFR-mutant non-small cell lung cancer cells. Fu, H; Fu, L; Li, Y; Lou, L; Quan, H; Zhang, M, 2021) | 1.11 |
| "To evaluate the potential gastric pH-dependent drug-drug interaction (DDI), safety and tolerability of famitinib co-administered with omeprazole in healthy subjects." | ( Phase I study to evaluate of the gastric pH-dependent drug interaction between famitinib and the proton pump inhibitor omeprazole in healthy subjects. Cai, M; Dou, T; Hu, L; Qian, W; Sun, Q; Tang, L; Wang, H, 2022) | 1.16 |
Oral famitinib bioavailability is not affected by food intake. Patients with cancer do not need to consider dietary status when using famit inib.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Famitinib is well absorbed and extensively metabolized in cancer patients." | ( Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Chen, X; Diao, X; Gao, Z; Guo, Z; Jiang, H; Xie, C; Zhang, L; Zhong, D; Zhou, J, 2013) | 2.12 |
| " In conclusion, oral famitinib bioavailability is not affected by food intake, implying that patients with cancer do not need to consider dietary status when using famitinib." | ( Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants. Li, S; Rao, J; Shi, G; Wen, Q; Zhang, X; Zhao, H, 2023) | 1.44 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Blood samples were collected before dosing (0 hour) to 192 hours after dosing, and famitinib concentrations in plasma were determined with validated liquid chromatography-tandem mass spectrometry." | ( Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants. Li, S; Rao, J; Shi, G; Wen, Q; Zhang, X; Zhao, H, 2023) | 1.35 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0040 | 0.0006 | 0.8007 | 8.5000 | AID536881 |
| Mast/stem cell growth factor receptor Kit | Homo sapiens (human) | IC50 (µMol) | 0.0020 | 0.0007 | 0.4708 | 10.0000 | AID536879 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0035 | 0.0000 | 0.4830 | 8.8000 | AID536880; AID536882 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 12 (50.00) | 24.3611 |
| 2020's | 12 (50.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (29.50) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 10 (41.67%) | 5.53% |
| Reviews | 1 (4.17%) | 6.00% |
| Case Studies | 1 (4.17%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 12 (50.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||